Betahistine Dihydrochloride Tablets 8mg Taj Pharma

  1. NAME OF THE MEDICINAL PRODUCT

Betahistine Dihydrochloride Tablets 8mg Taj Pharma
Betahistine Dihydrochloride Tablets 16mg Taj Pharma
Betahistine Dihydrochloride Tablets 24mg Taj Pharma

  1. QUALITATIVE AND QUANTITATIVE COMPOSITION
     a) Each uncoated tablet contains:
    Betahistine Dihydrochloride               8mg
    Excipients                                             q.s.
    b) Each uncoated tablet contains:
    Betahistine Dihydrochloride               16mg
    Excipients                                              q.s.
    c) Each uncoated tablet contains:
    Betahistine Dihydrochloride               24mg
    Excipients                                              q.s.

For the full list of excipients, see section 6.1.

  1. PHARMACEUTICAL FORM

Tablet.

  1. CLINICAL PARTICULARS

4.1 Therapeutic indications

Betahistine Dihydrochloride is indicated for the treatment of Ménière’s syndrome, symptoms of which may include vertigo, tinnitus, hearing loss and nausea

4.2 Posology and method of administration

Dosage

Adults:

Initial oral treatment is 8 to 8mg/16mg/24mg three times daily, taken preferably with meals.

Maintenance doses are generally in the range 24 – 48 mg daily. Daily dose should not exceed 48 mg. Dosage can be adjusted to suit individual patient needs. Sometimes improvement could be observed only after a couple of weeks of treatment.

Renal impairment

There are no specific clinical trials available in this patient group, but according to post-marketing experience no dose adjustment appears to be necessary.

Hepatic impairment

There are no specific clinical trials available in this patient group, but according to post-marketing experience no dose adjustment appears to be necessary.

Elderly population

Although there are limited data from clinical studies in this patient group, extensive post marketing experience suggests that no dose adjustment is necessary in this population.

Paediatric population:

Betahistine Dihydrochloride tablets are not recommended for use in children and adolescents below age 18 due to lack of data on safety and efficacy.

Method of administration

Take the tablets preferably with meals or after meals with a glass of water.

4.3 Contraindications

Hypersensitivity to the active substance(s) or to any of the excipients listed in section 6.1

Betahistine Dihydrochloride is contraindicated in patients with phaeochromocytoma. As Betahistine Dihydrochloride is a synthetic analogue of histamine it may induce the release of catecholamines from the tumor resulting in severe hypertension.

4.4 Special warnings and precautions for use

Caution is advised in the treatment of patients with peptic ulcer or a history of peptic ulceration, because of the occasional dyspepsia encountered in patients on Betahistine Dihydrochloride.

Patients with bronchial asthma should be monitored carefully during the treatment with Betahistine Dihydrochloride.

Caution is advised in prescribing Betahistine Dihydrochloride to patients with either urticaria, rashes or allergic rhinitis, because of the possibility of aggravating these symptoms.

Caution is advised in patients with severe hypotension.

4.5 Interaction with other medicinal products and other forms of interaction

There are no proven cases of hazardous interactions. No in-vivo interaction studies have been performed. Based on in-vitro data no in-vivo inhibition on Cytochrome P450 enzymes is expected.

Although an antagonism between Betahistine Dihydrochloride and antihistamines could be expected on a theoretical basis, no such interactions have been reported.

There is a case report of an interaction with ethanol and a compound containing pyrimethamine with dapsone and another of potentiation of Betahistine Dihydrochloride with salbutamol.

In vitro data indicate an inhibition of Betahistine Dihydrochloride metabolism by drugs that inhibit monoamino-oxidase (MAO) including MAO subtype B (e.g. selegiline). Caution is recommended when using Betahistine Dihydrochloride and MAO inhibitors (including MAO-B selective) concomitantly.

Betahistine Dihydrochloride is a histamine analogue, concurrent administration of H1 antagonists may cause a mutual attenuation of effect of the active agents.

4.6 Fertility, pregnancy and lactation

Pregnancy

There is a very limited amount of data from the use of Betahistine Dihydrochloride in pregnant women. Animal studies, though insuffcient do not indicate direct or indirect harmful effects with respect to reproductive toxicity (see section 5.3). The potential risk for humans is unknown. As a precautionary measure, it is preferable to avoid the use of Betahistine Dihydrochloride during pregnancy.

Lactation

There is insufficient information on the excretion of Betahistine Dihydrochloride in human milk. There are no animal studies on the excretion of Betahistine Dihydrochloride in milk. Betahistine Dihydrochloride should not be used during breastfeeding.

4.7 Effects on ability to drive and use machines

Betahistine Dihydrochloride is indicated for vertigo, tinnitus and hearing loss associated with Ménière’s syndrome which can negatively affect the ability to drive and use machines. In clinical studies specifically designed to investigate the ability to drive and use machines, Betahistine Dihydrochloride had no or negligible effects.

4.8 Undesirable effects

The following undesirable effects have been experienced with the below indicated frequencies in Betahistine Dihydrochloride-treated patients in placebo-controlled clinical trials and in post-marketing reports: very common (≥ 1/10); common (≥ 1/100 to <1/10); uncommon (≥ 1/1,000 to <1/100); rare ( ≥1/10,000 to <1/1,000); very rare (<1/10,000); and not known (frequency cannot be estimated from the available data).

Gastrointestinal disorders:
Common: nausea & dyspepsia
Nervous system disorders:
Common: headache
In addition to those events reported during clinical trials, the following undesirable effects have been reported spontaneously during post-marketing use and in scientific literature. A frequency cannot be estimated from the available data and is therefore classified as “not known”.
Immune system disorders:
Not known: hypersensitivity reactions, e.g. anaphylaxis.
Gastrointestinal disorders:
Not known: Mild gastric complaints (e.g. vomiting, gastrointestinal pain, abdominal distension and bloating). These can normally be dealt with by taking the dose during meals or by lowering the dose.
Skin and subcutaneous tissue disorders
Not known: cutaneous and subcutaneous hypersensitivity reactions, in particular angioneurotic oedema, urticarial, rash, and pruritus


Reporting of suspected adverse reactions

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the Yellow Card Scheme at: www.mhra.gov.uk/yellowcard.

4.9 Overdose

A few overdose cases have been reported. Some patients experienced mild to moderate symptoms with doses up to 640 mg (e.g. nausea, somnolence, abdominal pain).Other symptoms of Betahistine Dihydrochloride overdose are vomiting, dyspepsia, ataxia and seizures. More serious complications (convulsion, pulmonary or cardiac complications) were observed in cases of intentional overdose of Betahistine Dihydrochloride especially in combination with other overdosed drugs. No specific antidote. Gastric lavage and symptomatic treatment are recommended within one hour after intake.

  1. PHARMACOLOGICAL PROPERTIES

5.1 Pharmacodynamic properties

Pharmacotherapeutic group: 2.7 Central Nervous System. Antiemetic and anti-vertigo

The mechanism of action of Betahistine Dihydrochloride is only partially understood.

There are several plausible hypotheses that are supported by animal studies and human data:

Betahistine Dihydrochloride affects the histaminergic system:

Betahistine Dihydrochloride acts both as a partial histamine H1-receptor agonist and histamine H3-receptor antagonist also in neuronal tissue, and has negligible H2-receptor activity.

Betahistine Dihydrochloride increases histamine turnover and release by blocking presynaptic H3-receptors and inducing H3-receptor downregulation.

Betahistine Dihydrochloride may increase blood flow to the cochlear region as well as to the whole brain:

Pharmacological testing in animals has shown that the blood circulation in the striae vascularis of the inner ear improves, probably by means of a relaxation of the precapillary sphincters of the microcirculation of the inner ear.

Betahistine Dihydrochloride was also shown to increase cerebral blood flow in humans.

Betahistine Dihydrochloride facilitates vestibular compensation:

Betahistine Dihydrochloride accelerates the vestibular recovery after unilateral neurectomy in animals, by promoting and facilitating central vestibular compensation; this effect is characterised by an up-regulation of histamine turnover and release, is mediated via the H3 Receptor antagonism.

In human subjects, recovery time after vestibular neurectomy was also reduced when treated with Betahistine Dihydrochloride.

Betahistine Dihydrochloride alters neuronal firing in the vestibular nuclei:

Betahistine Dihydrochloride was also found to have a dose-dependent inhibiting effect on spike generation of neurons in lateral and medial vestibular nuclei.

The pharmacodynamic properties as demonstrated in animals may contribute to the therapeutic benefit of Betahistine Dihydrochloride in the vestibular system.

The efficacy of Betahistine Dihydrochloride was shown in studies in patients with vestibular vertigo and with Ménière’s disease as was demonstrated by improvements in severity and frequency of vertigo attacks.

5.2 Pharmacokinetic properties

Absorption

Orally administered Betahistine Dihydrochloride is readily and almost completely absorbed from all parts of the gastro-intestinal tract. After absorption, the drug is rapidly and almost completely metabolized into 2-pyridylacetic acid. Plasma levels of Betahistine Dihydrochloride are very low. Pharmacokinetic analyses are therefore based on 2-PAA measurements in plasma and urine.

Under fed conditions Cmax is lower compared to fasted conditions. However, total absorption of Betahistine Dihydrochloride is similar under both conditions, indicating that food intake only slows down the absorption of Betahistine Dihydrochloride.

Distribution

The percentage of Betahistine Dihydrochloride that is bound by blood plasma proteins is less than 5 %.

Biotransformation

After absorption, Betahistine Dihydrochloride is rapidly and almost completely metabolised into 2-PAA (which has no pharmacological activity).

After oral administration of Betahistine Dihydrochloride the plasma (and urinary) concentration of 2-PAA reaches its maximum 1 hour after intake and declines with a half-life of about 3.5 hours.

Excretion:

2-PAA is readily excreted in the urine. In the dose range between 8 and 48 mg, about 85% of the original dose is recovered in the urine. Renal or fecal excretion of Betahistine Dihydrochloride itself is of minor importance.

Linearity:

Recovery rates are constant over the oral dose range of 8 – 48 mg indicating that the pharmacokinetics of Betahistine Dihydrochloride are linear, and suggesting that the involved metabolic pathway is not saturated.

5.3 Preclinical safety data

Repeated dose toxicity studies of six months duration in dogs and 18 months duration in albino rats revealed no clinically relevant harmful effects at dose levels in the range 2.5 to 120 mg. kg –1. Betahistine Dihydrochloride is devoid of mutagenic potential and there was no evidence of carcinogenicity in rats. Tests conducted on pregnant rabbits showed no evidence of teratological effects.

           6. PHARMACEUTICAL PARTICULARS

a) Each uncoated tablet contains:
Betahistine Dihydrochloride               8mg
Excipients                                             q.s.

b) Each uncoated tablet contains:
Betahistine Dihydrochloride               16mg
Excipients                                              q.s.

c) Each uncoated tablet contains:
Betahistine Dihydrochloride               24mg
Excipients                                              q.s.

6.1 List of excipients

Microcrystalline cellulose, Mannitol, Povidone, Crospovidone, Citric acid anhydrous, Colloidal anhydrous silica, Talc, Stearic acid

6.2 Incompatibilities

Not applicable.

6.3 Shelf life

2 years.

6.4 Special precautions for storage

This medicinal product does not require any special storage conditions.

6.5 Nature and contents of container

PVC/PVDC/Al blisters.

Pack sizes: Blisters: 7, 14, 28, 30, 50, 90, 100 and 500mg modified-release tablets.

Not all pack sizes may be marketed.

6.6 Special precautions for disposal and other handling

No special requirements.

  1. MANUFACTURED IN INDIA BY:

TAJ PHARMACEUTICALS LTD.
Mumbai, India
Unit No. 214.Old Bake House,
Maharashtra chambers of  Commerce Lane,
Fort, Mumbai – 400001
at:Gujarat, INDIA.
Customer Service and Product Inquiries:
1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
E-mail: tajgroup@tajpharma.com

Betahistine Tablets Taj Pharma

Package leaflet: Information for the user
Betahistine Dihydrochloride 8mg, 16mg, 24mg tablets
Read all of this leaflet carefully before you start taking this medicine because it contains important information for you.

  • Keep this leaflet. You may need to read it again.
  • If you have any further questions, ask your doctor or pharmacist.
  • This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours.
  • If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4.

WHAT IS IN THIS LEAFLET

  1. What Betahistine is and what it is used for
  2. What you need to know before you take Betahistine
  3. How to take Betahistine
  4. Possible side effects
  5. How to store Betahistine
  6. Contents of the pack and other information1. WHAT BETAHISTINE IS AND WHAT IT IS USED FOR

Betahistine is a type of medicine called a “histamine analogue”.
Betahistine is used for: Ménière’s disease – the signs of this include:

  • feeling dizzy (vertigo)
  • ringing in the ears (tinnitus)
  • hearing loss or hearing difficulty

This medicine works by improving blood flow in the inner ear. This lowers the buildup of pressure.

  1. WHAT YOU NEED TO KNOW BEFORE YOU TAKE BETAHISTINE

Do not take Betahistine

  • if you are allergic to betahistine or to any of the other ingredients of this medicine (listed in section 6)
  • if you have a pheochromocytoma, a rare tumour of the adrenal gland

Warnings and precautions

Talk to your doctor or pharmacist before taking Betahistine.

  • if you have a stomach ulcer (peptic ulcer)
  • if you have asthma
  • if you have nettle rash, skin rash or a cold in the nose caused by an allergy, since these complaints may be exacerbated.
  • if you have low blood pressure

If you suffer from any of the above conditions, consult your doctor about whether you may take Betahistine tablets.

These groups of patients should be monitored by a doctor during treatment.

Children

Betahistine is not recommended for those under 18 years old.

Other medicines and Bethisitine

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.

In particular, tell your doctor or pharmacist if you are taking any of the following medicines:

Anti-histamines – This is because in theory betahistine may not work properly. Also, betahistine may lower the effect of anti-histamines.

Monoamine-oxidase inhibitors (MAOIs) – used to treat depression or Parkinson’s disease. These may increase the exposure of betahistine.

If any of the above apply to you (or you are not sure), talk to your doctor or pharmacist before taking Betahistine.

Taking Betahistine with food and drink

Betahistine can be taken with or without food. However, Betahistine can cause mild stomach problems (listed in section 4). Taking betahistine with food can help reduce stomach problems.

Pregnancy, breast-feeding and fertility

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine.

Do not take betahistine dihydrochloride tablets if you are pregnant unless your doctor has decided that it is absolutely necessary. Ask your doctor for advice.

Do not breast-feed while using betahistine dihydrochloride tablets unless instructed by your doctor. It is not known if betahistine passes into breast milk.

Driving and using machines

Betahistine is not likely to affect your ability to drive or use tools or machinery.

However, remember that the disease for which you are being treated with Betahistine (Ménière’s disease) can make you feel dizzy or sick, and can affect your ability to drive and use machines.

  1. HOW TO TAKE BETAHISTINE

Always take this medicine exactly as your doctor or pharmacist has told you. Check with your doctor or pharmacist if you are not sure.

  • Your doctor will adjust your dose, depending on your progress.
  • Keep taking your medicine. The medicine can take a while to start to work.

How to take Betahistine

  • Swallow the tablets with water.
  • Take the tablet with or after a meal. However, Betahistine can cause mild stomach problems (listed in Section 4). Taking Betahistine with food can help reduce stomach problems.

How much Betahistine to take

Always follow your doctor’s instructions because your doctor might adjust your dose.

The recommended dose is:

Adults

The recommended dose is 24 mg to 48mg, 16mg, 24mg per day. 8mg, 16mg, 24mg tablets: one or two tablets three times a day.

16 mg tablets: half or one tablet three times a day.

If you take more than one tablet each day, spread your tablets evenly over the day. For example, take one tablet in the morning, one at midday and one in the evening.

Try to take your tablet at the same time each day. This will make sure that there is a steady amount of the medicine in your body. Taking at the same time will also help you remember to take your tablets. Betahistine is not recommended for use in children.

If you take more Betahistine than you should

If you or someone else takes too many Betahistine tablets (an overdose), you may feel sick (nauseous), sleepy or have stomach pain. Talk to a doctor or go to a hospital immediately. Take the Betahistine pack with you.

If you forget to take Betahistine

Wait until you have to take your next dose. Do not take a double dose to make up for a forgotten tablet.

If you stop taking Betahistine

Keep taking your tablets until your doctor tells you to stop.

Even when you start feeling better, your doctor may want you to carry on taking the tablets for some time to make sure that the medicine has worked completely.

If you have any further questions on the use of this medicine, ask your doctor or pharmacist.

  1. POSSIBLE SIDE EFFECTS

Like all medicines, this medicine can cause side effects, although not everybody gets them. Very few adverse effects have been reported with betahistine.

The following serious side effects may occur during treatment with Betahistine:

Allergic reactions:

  • a red or lumpy skin rash or inflamed itchy skin
  • swelling of your face, lips, tongue or neck
  • a drop in your blood pressure
  • loss of consciousness
  • difficulty breathing

If any of these side effects occur you should stop treatment immediately and contact your doctor.

Other side effects include:

Common (may affect up to 1 in 10 people):

  • feeling sick (nausea)
  • indigestion (dyspepsia)

Other side effects that have been reported with the use of betahistine

Mild stomach problems such as being sick (vomiting), stomach pain, stomach swelling (abdominal distension) and bloating. Taking betahistine with food can help reduce stomach problems.

Reporting of side effects

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet.

  1. HOW TO STORE BETAHISTINE

Keep this medicine out of the sight and reach of children.

This medicinal product does not require any special storage conditions.

Do not use this medicine after the expiry date which is stated on the label, carton, bottle after (EXP).The expiry date refers to the last day of that month.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.

  1. CONTENTS OF THE PACK AND OTHER INFORMATION

What Betahistine contains

a) Each uncoated tablet contains:
Betahistine Dihydrochloride               8mg
Excipients                                             s.

b) Each uncoated tablet contains:
Betahistine Dihydrochloride               16mg
Excipients                                             s.

c) Each uncoated tablet contains:
Betahistine Dihydrochloride               24mg
Excipients                                           s.

The other ingredients are microcrystalline cellulose, mannitol, povidone, crospovidone, citric acid anhydrous, colloidal anhydrous silica, talc and stearic acid.

What Betahistine looks like and the contents of the pack

Tablet.

Betahistine 8mg, 16mg, 24mg tablets

Betahistine Tablets are available in:

PVC/PVDC/Al blisters.

Pack sizes: Blisters: 7, 14, 28, 30, 50, 90, 100 and 500mg modified-release tablets.

Not all pack sizes may be marketed.

  1. MANUFACTURED IN INDIA BY:TAJ PHARMACEUTICALS LTD.
    Mumbai, India
    Unit No. 214.Old Bake House,
    Maharashtra chambers of  Commerce Lane,
    Fort, Mumbai – 400001
    at:Gujarat, INDIA.
    Customer Service and Product Inquiries:
    1-800-TRY-FIRST (1-800-222-434 & 1-800-222-825)
    Monday through Saturday 9:00 a.m. to 7:00 p.m. EST
    E-mail: tajgroup@tajpharma.com

 

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